Nanocrystals of a new camptothecin derivative WCN-21 enhance its solubility and efficacy.

ABSTRACT: WCN-21 is a new camptothecin derivative we synthesized and has desirable anti-tumor efficacy, but its aqueous solubility is very low and hurdles the further evaluation and development. In this study, we prepared nanocrystals of WCN-21 through a bottom-up approach to enhance its solubility and obtained WCN-21 nanorods (WND) and nanospheres (WNP). We investigated the crystallization of WND and WNP in different temperature and solvents and found that both temperature and solvents affect the crystal shapes and sizes. We prepared WND at 50°C and DMSO : H2O 1: 50 and WNP at 25°C and DMSO : H2O 1: 100 and found they were dispersed evenly in water with average hydrodynamic diameters 337 and 231 nm, respectively. WND and WNP increased the solubility of WCN-21 from extreme insolubility to more than

SUBMITTER: You J 

PROVIDER: S-EPMC5444705 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature